David W Nash

US Patent:

20040242575, Dec 2, 2004

Filed:

Jul 2, 2004

Appl. No.:

10/492250

Inventors:

Clive Branch - King of Prussia PA, US
Chirstopher Johnson - King of Prussia PA, US
David Nash - King of Prussia PA, US
Geoffrey Stemp - King of Prussia PA, US

International Classification:

A61K031/541
A61K031/5377
A61K031/496
A61K031/495
C07D417/02
C07D413/02
C 07D 4 3/02

US Classification:

514/227800, 514/235500, 514/253110, 514/255010, 544/060000, 544/114000, 544/360000, 544/386000

Abstract:

This invention relates to N-aroyl piperazine derivatives of formula (I), wherein: Y represents NR; m represents 1, 2 or 3; p represents 0 or 1; X is O, S, C O, SO, or CH CH—; Aris aryl, or a mono or bicyclic heteroaryl group containing up to 4 heteroatoms selected from N, O and S; any of which may be optionally substituted; Arrepresents phenyl or a 5- or 6-membered heterocyclyl group containing 1 to 3 heteroatoms selected from N, O and S, wherein the phenyl heterocyclyl group is substituted by Rand further optional substituents; or Arrepresents an optionally substituted bicyclic aromatic or bicyclic heteroaromatic group containing 1 to 4 heteroatoms selected from N, O and S; Rrepresents optionally substituted (C)alkoxy, halo, optionally substituted (C)alkyl, optionally substituted phenyl, or an optionally substituted 5- or 6-membered heterocyclic ring containing 1 to 4 heteroatoms selected from N, O and S; R?2 represents hydrogen, optionally substituted (C)alkyl, optionally substituted (C)alkanoyl, optionally subtituted (C)alkanoxycarbonyl or optionally substituted aryl(C)alkyloxycarbonyl; and their use as orexin receptor-antagonists.